MLCK
抑制剂选择性比较
MLCK产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1573 |
Fasudil (HA-1077) HClFasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
![]() ![]() The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
|
S3699 |
2,3-Butanedione-2-monoxime2,3-Butanedione monoxime (BDM, Diacetyl monoxime, Diacetylmonoxime) 是一种低亲和力的、非竞争性的skeletal muscle myosin-II抑制剂,抑制骨骼肌和心肌收缩。 |
||
S8388 |
ML-7 HClML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂,Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC,对应的Ki值分别为21 μM和42 μM。 |
![]() ![]() Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
|
|
S6847 |
ML-9 HClML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。 |
||
S2964 |
HA-100 dihydrochlorideHA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂,对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。 |
||
S8861 |
Mavacamten (MYK-461)Mavacamten (MYK-461, SAR439152)是心肌肌球蛋白(cardiac myosin)的小分子调节剂,调节肥厚型心肌病的肌节过强收缩。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1573 |
Fasudil (HA-1077) HClFasudil (HA-1077, AT-877)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
![]() ![]() The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
|
S3699 |
2,3-Butanedione-2-monoxime2,3-Butanedione monoxime (BDM, Diacetyl monoxime, Diacetylmonoxime) 是一种低亲和力的、非竞争性的skeletal muscle myosin-II抑制剂,抑制骨骼肌和心肌收缩。 |
||
S8388 |
ML-7 HClML-7 是平滑肌肌球蛋白轻链激酶MLCK抑制剂,Ki值为0.3 μM。对钙离子-钙调蛋白依赖性或非依赖性的平滑肌MLCKs具有可逆的、ATP竞争性抑制作用。ML-7 还可抑制 PKA 和 PKC,对应的Ki值分别为21 μM和42 μM。 |
![]() ![]() Platelets (3 × 108/mL) were treated with ML-7 (5 µM) for 20 minutes, followed by stimulation with oxLDL (50 µg/mL) for 15 seconds. Samples were then lysed, separated by SDS-PAGE, and immunoblotted for phospho-MLCSer19 followed by reprobing for β-tubulin. (Ai) Representative blots. (Aii) Densitometric analysis of 5 independent experiments. *P < .05.
|
|
S6847 |
ML-9 HClML-9 HCl (ML-9 hydrochloride) 是一种有效的选择性的 Akt kinase、myosin light chain kinase (MLCK) 和 stromal interaction molecule 1 (STIM1)。ML-9 HCl 也是 Ca2+-permeable channels 的有效抑制剂。ML-9 HCl 是一种靶向自噬和细胞死亡的亲溶酶体剂。 |
||
S2964 |
HA-100 dihydrochlorideHA-100 dihydrochloride 是 cGMP-dependent protein kinase (PKG)、cAMP-dependent protein kinase (PKA)、protein kinase C (PKC) 和 MLC-kinase 的抑制剂,对应的IC50值分别为4 μM、8 μM、12 μM和240 μM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8861 |
Mavacamten (MYK-461)Mavacamten (MYK-461, SAR439152)是心肌肌球蛋白(cardiac myosin)的小分子调节剂,调节肥厚型心肌病的肌节过强收缩。 |